CN102740851B - Pi3k抑制剂和mek抑制剂的组合 - Google Patents

Pi3k抑制剂和mek抑制剂的组合 Download PDF

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Publication number
CN102740851B
CN102740851B CN2010800563069A CN201080056306A CN102740851B CN 102740851 B CN102740851 B CN 102740851B CN 2010800563069 A CN2010800563069 A CN 2010800563069A CN 201080056306 A CN201080056306 A CN 201080056306A CN 102740851 B CN102740851 B CN 102740851B
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gdc
patient
tumor
compound
formula
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Chinese (zh)
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CN102740851A (zh
Inventor
M.贝尔文
I.T.钱
L.弗里德曼
K.P.霍夫利科
J.普雷斯科特
J.沃林
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F Hoffmann La Roche AG
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CN2010800563069A 2009-10-12 2010-10-11 Pi3k抑制剂和mek抑制剂的组合 Expired - Fee Related CN102740851B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US25085209P 2009-10-12 2009-10-12
US61/250,852 2009-10-12
PCT/EP2010/065149 WO2011054620A1 (en) 2009-10-12 2010-10-11 Combinations of a pi3k inhibitor and a mek inhibitor

Publications (2)

Publication Number Publication Date
CN102740851A CN102740851A (zh) 2012-10-17
CN102740851B true CN102740851B (zh) 2013-12-18

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CN2010800563069A Expired - Fee Related CN102740851B (zh) 2009-10-12 2010-10-11 Pi3k抑制剂和mek抑制剂的组合

Country Status (24)

Country Link
US (1) US20110086837A1 (https=)
EP (1) EP2488178B1 (https=)
JP (2) JP2013507415A (https=)
KR (1) KR101489045B1 (https=)
CN (1) CN102740851B (https=)
AR (1) AR078588A1 (https=)
AU (1) AU2010314287A1 (https=)
BR (1) BR112012008483A2 (https=)
CA (1) CA2776944A1 (https=)
CL (1) CL2012000913A1 (https=)
CO (1) CO6531463A2 (https=)
CR (1) CR20120173A (https=)
EC (1) ECSP12011865A (https=)
ES (1) ES2609767T3 (https=)
IL (1) IL219105A0 (https=)
MA (1) MA33974B1 (https=)
MX (1) MX345155B (https=)
NZ (1) NZ599939A (https=)
PE (1) PE20121816A1 (https=)
PH (1) PH12012500709A1 (https=)
RU (1) RU2563193C2 (https=)
TW (1) TWI428336B (https=)
WO (1) WO2011054620A1 (https=)
ZA (1) ZA201202618B (https=)

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EA024252B1 (ru) 2009-01-08 2016-08-31 Кьюрис, Инк. Ингибиторы фосфоинозитид-3-киназ с цинксвязывающей группой
PH12012501361A1 (en) 2009-12-31 2012-10-22 Centro Nac De Investigaciones Oncologicas Cnio Tricyclic compounds for use as kinase inhibitors
WO2012098387A1 (en) 2011-01-18 2012-07-26 Centro Nacional De Investigaciones Oncológicas (Cnio) 6, 7-ring-fused triazolo [4, 3 - b] pyridazine derivatives as pim inhibitors
WO2012135571A1 (en) 2011-04-01 2012-10-04 Curis, Inc. Phosphoinositide 3-kinase inhibitor with a zinc binding moiety
MX368257B (es) 2011-08-01 2019-09-26 Genentech Inc Antagonistas de unión al eje pd-1e inhibidores de mek y sus usos en el tratamiento de cáncer.
KR20140072028A (ko) * 2011-08-31 2014-06-12 노파르티스 아게 Pi3k- 및 mek-억제제의 상승작용적 조합물
CA2849331A1 (en) 2011-10-13 2013-04-18 Genentech, Inc. Treatment of pharmacological-induced hypochlorhydria
MX2014004991A (es) * 2011-10-28 2014-05-22 Genentech Inc Combinaciones terapeuticas y metodos para tratar el melanoma.
WO2013082511A1 (en) 2011-12-02 2013-06-06 Genentech, Inc. Methods for overcoming tumor resistance to vegf antagonists
AU2013243429A1 (en) * 2012-04-06 2014-10-23 Merck Patent Gmbh Methods for treating cancer using PI3K inhibitor and MEK inhibitor
WO2013157648A1 (ja) * 2012-04-19 2013-10-24 国立大学法人九州大学 医薬組成物
BR112014028376A2 (pt) 2012-06-08 2018-04-24 Hoffmann La Roche métodos para o tratamento de um distúrbio hiperproliferativo, para a determinação dos compostos, para monitorar, para optimizar a eficácia terapêutica e de identificação de um biomarcador; formulação farmacêutica; utilização de uma combinação terapêutica e de gdc-0032, artigo de manufatura, produto e invenção
CA2879670A1 (en) 2012-08-02 2014-02-06 Genentech, Inc. Anti-etbr antibodies and immunoconjugates
JP2015528818A (ja) 2012-08-02 2015-10-01 ジェネンテック， インコーポレイテッド 抗ｅｔｂｒ抗体およびイムノコンジュゲート
KR20190057421A (ko) 2012-08-17 2019-05-28 에프. 호프만-라 로슈 아게 코비메티닙 및 베무라피닙을 투여함을 포함하는 흑색종의 조합 치료법
MX2015010854A (es) * 2013-03-14 2016-07-20 Genentech Inc Combinaciones de un compuesto inhibidor de mek con un compuesto inhibidor de her3/egfr y metodos de uso.
US9532987B2 (en) 2013-09-05 2017-01-03 Genentech, Inc. Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases
WO2015120289A1 (en) 2014-02-07 2015-08-13 Verastem, Inc. Methods and compositions for treating abnormal cell growth
EP3563870A1 (en) 2014-07-15 2019-11-06 F. Hoffmann-La Roche AG Methods of treating cancer using pd-1 axis binding antagonists and mek inhibitors
CN113620978A (zh) * 2014-09-11 2021-11-09 加利福尼亚大学董事会 mTORC1抑制剂
CN113164466B (zh) 2018-09-11 2025-07-08 柯瑞斯公司 使用具有锌结合部分的磷酸肌醇3-激酶抑制剂的联合治疗
CN110420330B (zh) * 2019-07-19 2020-05-29 南京医科大学 一种pi3k与mth1靶向药组合物的制药用途
JP2022547358A (ja) 2019-09-13 2022-11-14 ジ インスティテュート オブ キャンサー リサーチ：ロイヤル キャンサー ホスピタル 治療組成物、組み合わせ、及び使用方法
US11873296B2 (en) 2022-06-07 2024-01-16 Verastem, Inc. Solid forms of a dual RAF/MEK inhibitor

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WO2007129161A2 (en) * 2006-04-26 2007-11-15 F. Hoffmann-La Roche Ag Thieno [3, 2-d] pyrimidine derivative useful as pi3k inhibitor
WO2008070740A1 (en) * 2006-12-07 2008-06-12 F.Hoffmann-La Roche Ag Phosphoinositide 3-kinase inhibitor compounds and methods of use

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WO2007129161A2 (en) * 2006-04-26 2007-11-15 F. Hoffmann-La Roche Ag Thieno [3, 2-d] pyrimidine derivative useful as pi3k inhibitor
WO2008070740A1 (en) * 2006-12-07 2008-06-12 F.Hoffmann-La Roche Ag Phosphoinositide 3-kinase inhibitor compounds and methods of use

Also Published As

Publication number Publication date
JP5745678B2 (ja) 2015-07-08
EP2488178B1 (en) 2016-11-16
CA2776944A1 (en) 2011-05-12
PE20121816A1 (es) 2013-01-02
NZ599939A (en) 2014-02-28
ZA201202618B (en) 2014-10-29
KR101489045B1 (ko) 2015-02-02
AR078588A1 (es) 2011-11-16
JP2015038110A (ja) 2015-02-26
US20110086837A1 (en) 2011-04-14
HK1175125A1 (en) 2013-06-28
MA33974B1 (fr) 2013-02-01
BR112012008483A2 (pt) 2019-09-24
CN102740851A (zh) 2012-10-17
AU2010314287A2 (en) 2012-07-12
TW201118082A (en) 2011-06-01
CR20120173A (es) 2012-07-04
PH12012500709A1 (en) 2012-10-29
ECSP12011865A (es) 2012-06-29
KR20120064132A (ko) 2012-06-18
EP2488178A1 (en) 2012-08-22
MX2012004286A (es) 2012-05-22
RU2563193C2 (ru) 2015-09-20
CL2012000913A1 (es) 2012-09-14
ES2609767T3 (es) 2017-04-24
CO6531463A2 (es) 2012-09-28
WO2011054620A1 (en) 2011-05-12
TWI428336B (zh) 2014-03-01
IL219105A0 (en) 2012-06-28
JP2013507415A (ja) 2013-03-04
AU2010314287A1 (en) 2012-05-03
RU2012118974A (ru) 2013-11-20
MX345155B (es) 2017-01-18

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